EP3551610A4 - Inhibiteurs bicyclo[1.1.1]pentane de la double fermeture à glissière de leucine kinase (dlk) destinés au traitement de maladie - Google Patents

Inhibiteurs bicyclo[1.1.1]pentane de la double fermeture à glissière de leucine kinase (dlk) destinés au traitement de maladie Download PDF

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Publication number
EP3551610A4
EP3551610A4 EP17879488.9A EP17879488A EP3551610A4 EP 3551610 A4 EP3551610 A4 EP 3551610A4 EP 17879488 A EP17879488 A EP 17879488A EP 3551610 A4 EP3551610 A4 EP 3551610A4
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EP
European Patent Office
Prior art keywords
dlk
bicyclo
leucine
pentane
kinase
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Granted
Application number
EP17879488.9A
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German (de)
English (en)
Other versions
EP3551610A1 (fr
EP3551610B1 (fr
Inventor
Michael J. SOTH
Gang Liu
Kang Le
Jason Cross
Philip Jones
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
University of Texas System
University of Texas at Austin
Original Assignee
University of Texas System
University of Texas at Austin
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Publication of EP3551610A1 publication Critical patent/EP3551610A1/fr
Publication of EP3551610A4 publication Critical patent/EP3551610A4/fr
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Epidemiology (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
EP17879488.9A 2016-12-08 2017-12-08 Inhibiteurs bicyclo[1.1.1]pentane de la double fermeture à glissière de leucine kinase (dlk) destinés au traitement de maladie Active EP3551610B1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201662431504P 2016-12-08 2016-12-08
PCT/US2017/065385 WO2018107072A1 (fr) 2016-12-08 2017-12-08 Inhibiteurs bicyclo[1.1.1]pentane de la double fermeture à glissière de leucine kinase (dlk) destinés au traitement de maladie

Publications (3)

Publication Number Publication Date
EP3551610A1 EP3551610A1 (fr) 2019-10-16
EP3551610A4 true EP3551610A4 (fr) 2020-04-22
EP3551610B1 EP3551610B1 (fr) 2021-08-11

Family

ID=62492159

Family Applications (1)

Application Number Title Priority Date Filing Date
EP17879488.9A Active EP3551610B1 (fr) 2016-12-08 2017-12-08 Inhibiteurs bicyclo[1.1.1]pentane de la double fermeture à glissière de leucine kinase (dlk) destinés au traitement de maladie

Country Status (17)

Country Link
US (3) US10093664B2 (fr)
EP (1) EP3551610B1 (fr)
JP (1) JP7128816B2 (fr)
KR (1) KR20190087622A (fr)
CN (1) CN110191878B (fr)
AU (1) AU2017371084B2 (fr)
BR (1) BR112019011801A2 (fr)
CA (1) CA3045947A1 (fr)
CL (1) CL2019001539A1 (fr)
CO (1) CO2019006785A2 (fr)
EA (1) EA201991375A1 (fr)
EC (1) ECSP19048477A (fr)
ES (1) ES2895257T3 (fr)
IL (1) IL267121B (fr)
MX (1) MX386838B (fr)
WO (1) WO2018107072A1 (fr)
ZA (1) ZA201904402B (fr)

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JP7128816B2 (ja) 2016-12-08 2022-08-31 ボード オブ レジェンツ，ザ ユニバーシティ オブ テキサス システム 疾患の治療のための二重ロイシンジッパー（ｄｌｋ）キナーゼのビシクロ［１．１．１］ペンタン阻害剤
CA3071024A1 (fr) 2017-08-09 2019-02-14 Denali Therapeutics Inc. Composes, compositions et procedes
CN111201245B (zh) 2017-09-01 2024-04-05 戴纳立制药公司 化合物、组合物和方法
US20190382396A1 (en) * 2018-06-13 2019-12-19 Board Of Regents, The University Of Texas System Salts of bicyclo[1.1.1]pentane inhibitors of dual leucine zipper (dlk) kinase for the treatment of disease
GB201811165D0 (en) * 2018-07-06 2018-08-29 Metrion Biosciences Ltd Novel compounds
WO2020027723A1 (fr) * 2018-08-01 2020-02-06 Agency For Science, Technology And Research Composés bicycliques utilisés en tant que modulateurs de kinase, procédés et utilisations de ceux-ci
WO2020113094A1 (fr) 2018-11-30 2020-06-04 Nuvation Bio Inc. Composés pyrrole et pyrazole et leurs procédés d'utilisation
WO2020132045A1 (fr) 2018-12-19 2020-06-25 Disarm Therapeutics, Inc. Inhibiteurs de sarm1 en combinaison avec des agents neuroprotecteurs
SG11202108552QA (en) 2019-02-13 2021-09-29 Denali Therapeutics Inc Compounds, compositions and methods
EP3924341A4 (fr) 2019-02-13 2022-11-02 Denali Therapeutics Inc. Composés, compositions et procédés
IL291665B2 (en) * 2019-09-27 2025-07-01 Univ Texas Inhibitors of receptor interacting protein kinase i for the treatment of disease
US11560366B2 (en) * 2019-10-21 2023-01-24 Board Of Regents, The University Of Texas System Bicyclo[1.1.1]pentane inhibitors of dual leucine zipper (DLK) kinase for the treatment of disease
JP2023539754A (ja) * 2020-09-02 2023-09-19 ザ ユナイテッド ステイツ オブ アメリカ， アズ リプレゼンテッド バイ ザ セクレタリー， デパートメント オブ ヘルス アンド ヒューマン サービシーズ Ｌｚｋ標的化分解剤および使用方法
KR20240055041A (ko) 2021-09-01 2024-04-26 더 유나이티드 스테이츠 오브 아메리카, 애즈 레프리젠티드 바이 더 세크러테리, 디파트먼트 오브 헬스 앤드 휴먼 서비시즈 혼합 계통 키나제 억제제 및 억제제의 사용 방법
CN115974795A (zh) * 2022-12-26 2023-04-18 杭州师范大学 一种含全氟烷基和n杂环二取代双环[1.1.1]戊烷及其合成方法
WO2025021997A1 (fr) 2023-07-27 2025-01-30 Deutsches Krebsforschungszentrum Stiftung des öffentlichen Rechts Nouveaux inhibiteurs de map4k1

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WO2014111496A1 (fr) * 2013-01-18 2014-07-24 F. Hoffmann-La Roche Ag Pyrazoles 3 substitués et utilisation en tant qu'inhibiteurs de dlk
WO2015091889A1 (fr) * 2013-12-20 2015-06-25 F. Hoffmann-La Roche Ag Dérivés de pyrazole et leurs utilisations en tant qu'inhibiteurs de dlk
WO2018044808A1 (fr) * 2016-08-29 2018-03-08 Board Of Regents, University Of Texas System Inhibiteurs de la kinase à double motif de type glissière à leucines (dlk) destinés au traitement de maladie

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EP2852584B1 (fr) 2012-05-22 2018-02-28 F. Hoffmann-La Roche AG Dipyridylamines substituées et leurs utilisations
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PH12019502378A1 (en) 2013-05-01 2022-05-11 Hoffmann La Roche Biheteroaryl compounds and uses thereof
CA2907912A1 (fr) 2013-05-01 2014-11-06 F. Hoffmann-La Roche Ag Pyrimidines a substitution heterocycloalkyle liees a c et leurs utilisations
CA2942144C (fr) 2014-03-07 2023-08-22 Kalyra Pharmaceuticals, Inc. Derives de propellane et synthese
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HUE049481T2 (hu) 2015-04-03 2020-09-28 Recurium Ip Holdings Llc Spirociklusos vegyületek
JP7128816B2 (ja) 2016-12-08 2022-08-31 ボード オブ レジェンツ，ザ ユニバーシティ オブ テキサス システム 疾患の治療のための二重ロイシンジッパー（ｄｌｋ）キナーゼのビシクロ［１．１．１］ペンタン阻害剤
US11560366B2 (en) * 2019-10-21 2023-01-24 Board Of Regents, The University Of Texas System Bicyclo[1.1.1]pentane inhibitors of dual leucine zipper (DLK) kinase for the treatment of disease

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Publication number Priority date Publication date Assignee Title
WO2014111496A1 (fr) * 2013-01-18 2014-07-24 F. Hoffmann-La Roche Ag Pyrazoles 3 substitués et utilisation en tant qu'inhibiteurs de dlk
WO2015091889A1 (fr) * 2013-12-20 2015-06-25 F. Hoffmann-La Roche Ag Dérivés de pyrazole et leurs utilisations en tant qu'inhibiteurs de dlk
WO2018044808A1 (fr) * 2016-08-29 2018-03-08 Board Of Regents, University Of Texas System Inhibiteurs de la kinase à double motif de type glissière à leucines (dlk) destinés au traitement de maladie

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Title
See also references of WO2018107072A1 *

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IL267121A (en) 2019-08-29
US10428057B2 (en) 2019-10-01
CN110191878A (zh) 2019-08-30
AU2017371084A1 (en) 2019-06-20
US20180186781A1 (en) 2018-07-05
ECSP19048477A (es) 2019-07-31
JP2020502092A (ja) 2020-01-23
BR112019011801A2 (pt) 2019-10-29
US10093664B2 (en) 2018-10-09
CN110191878B (zh) 2023-05-26
CA3045947A1 (fr) 2018-06-14
MX386838B (es) 2025-03-19
CL2019001539A1 (es) 2019-08-23
US20220267311A1 (en) 2022-08-25
AU2017371084B2 (en) 2022-04-28
EA201991375A1 (ru) 2020-01-20
EP3551610A1 (fr) 2019-10-16
US20190092764A1 (en) 2019-03-28
ZA201904402B (en) 2020-12-23
CO2019006785A2 (es) 2019-07-10
ES2895257T3 (es) 2022-02-18
MX2019006645A (es) 2019-08-26
IL267121B (en) 2021-12-01
KR20190087622A (ko) 2019-07-24
EP3551610B1 (fr) 2021-08-11
WO2018107072A1 (fr) 2018-06-14
JP7128816B2 (ja) 2022-08-31

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